pH-Responsive Polycarbonate Copolymer-based Nanoparticles for Targeted Anticancer Drug Delivery  

作　　者：LI Yunxia DU Wenjuan FU Zhiguang WANG Huanhuan WANG Jiexin LE Yuan ZHANG Jianjun WEN Ning 

机构地区：[1]Department of Stomatology, the General Hospital of Chinese PLA, Beijing 100853, P. R. China [2]Department of Oncology, the General Hospital of Chinese PLA, Beijing 100853, P. R. China [3]College of Chemical Engineering, Beijing University of Chemical Technology, Beijing 100029, P. R. China

出　　处：《Chemical Research in Chinese Universities》2018年第6期1041-1050,共10页高等学校化学研究（英文版）

基　　金：Supported by the National High Technolgy Researeh and Development Program of China（No.2013AA032201）, the National Natural Science Foundation of China（Nos.81703003, 51303009, 21476018, 21622601） and the National Key R＆D Program of China（No.2015CB932101 ）.

摘　　要：A smart polycarbonate（PCA） copolymer-based nanoparticle（NanoPCA） with pH-responsive, long-term stability, and tumor targeting ability was successfully developed by synthesizing and assembling a series of functional PCA-based copolymers including poly（2-amino-l,3-propanediol carbonate-co-L-lactide）[P（CA-co-LA）], poly（2- amino-1,3-propanediol carbonate-co-L-lactide）-g-methoxy-poly（ethylene glycol）[P（CA-co-LA）-g-MPEG], and poly（2-amino-1,3-propanediol carbonate-co-L-lactide）-g-poly（ethylene glycol）-cyclic（Arg-Gly-Asp-D-Phe-Lys） [P（CA-co-LA）-g-PEG-cRGD] for targeted anticancer drug delivery, pH-Responsive studies demonstrated that the loading doxorubicin（DOX） released faster from NanoPCA at acidic conditions due to protonation effects of P（CA-co-LA） copolymers. Furthermore, the in vitro and in vivo investigations demonstrate that the DOX-loaded NanoPCA exhibited significant tumor targeting ability, outstanding antitumor effect and excellent biological safety in the treatment of oral squamous cell carcinoma（OSCC）. Therefore, this work provides a promising drug delivery plat-form for cancer therapy and other applications.A smart polycarbonate（PCA） copolymer-based nanoparticle（NanoPCA） with pH-responsive, long-term stability, and tumor targeting ability was successfully developed by synthesizing and assembling a series of functional PCA-based copolymers including poly（2-amino-l,3-propanediol carbonate-co-L-lactide）[P（CA-co-LA）], poly（2- amino-1,3-propanediol carbonate-co-L-lactide）-g-methoxy-poly（ethylene glycol）[P（CA-co-LA）-g-MPEG], and poly（2-amino-1,3-propanediol carbonate-co-L-lactide）-g-poly（ethylene glycol）-cyclic（Arg-Gly-Asp-D-Phe-Lys） [P（CA-co-LA）-g-PEG-cRGD] for targeted anticancer drug delivery, pH-Responsive studies demonstrated that the loading doxorubicin（DOX） released faster from NanoPCA at acidic conditions due to protonation effects of P（CA-co-LA） copolymers. Furthermore, the in vitro and in vivo investigations demonstrate that the DOX-loaded NanoPCA exhibited significant tumor targeting ability, outstanding antitumor effect and excellent biological safety in the treatment of oral squamous cell carcinoma（OSCC）. Therefore, this work provides a promising drug delivery plat-form for cancer therapy and other applications.

关 键 词：Polycarbonate copolymer-based nanoparticle（NanoPCA） PH-RESPONSIVE Tumor targeting ability Oral squamous cell carcinoma（OSCC） 

分 类 号：TP216[自动化与计算机技术—检测技术与自动化装置] O632.13[自动化与计算机技术—控制科学与工程]